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Showing 1–5 of 5 results
Advanced filters: Author: Jonathan M. L. Ostrem Clear advanced filters

  • Li et al. discovered that the cytotoxic synthetic small molecule BRD1732 is directly ubiquitinated in cells. Ubiquitination of BRD1732 is E3 ligase dependent and leads to inhibition of proteasomal degradation.

    • Weicheng Li
    • Enrique M. Garcia-Rivera
    • Jonathan M. L. Ostrem
    ResearchOpen Access
    Nature Chemical Biology
    P: 1-9

  • RAS proteins, central drivers of cancer, appeared ‘undruggable’ for almost 30 years. Here we provide a personal perspective on the effort leading to our initial report of KRASG12C inhibitors in 2013, and the decade of discoveries that followed.

    • Jonathan M. L. Ostrem
    • Ulf Peters
    • Kevan M. Shokat
    Comments & Opinion
    Nature Chemical Biology
    Volume: 20, P: 1238-1241

  • KRAS is one of the most frequently activated proteins in cancer, yet the development of RAS inhibitors has proven to be extremely challenging. Here, Shokat and Ostrem discuss the latest insights into RAS structure and dynamics, consider potential mechanisms of action for effective RAS inhibitors, and examine recent reports of direct RAS inhibitors.

    • Jonathan M. L. Ostrem
    • Kevan M. Shokat
    Reviews
    Nature Reviews Drug Discovery
    Volume: 15, P: 771-785

  • Small molecules are developed that irreversibly bind to the common G12C mutant of K-Ras but not the wild-type protein; crystallographic studies reveal the formation of an allosteric pocket that is not apparent in previous Ras studies, and the small molecules shift the affinity of K-Ras to favour GDP over GTP.

    • Jonathan M. Ostrem
    • Ulf Peters
    • Kevan M. Shokat
    Research
    Nature
    Volume: 503, P: 548-551